140481-05-6

ALKBH5-IN-5 (compound 18l) is an ALKBH5 inhibitor, exhibiting highly selective inhibitory effect on ALKBH5 with an IC50 of 0.62 μM. ALKBH5-IN-5 exerts a strong antiproliferative effect on NB4 cells with an IC50 of 0.63 μM. ALKBH5-IN-5 binds with ALKBH5 with a Kd of 804 nM. ALKBH5-IN-5 directly targets ALKBH5 in cells and alters m6A levels on mRNA, blocks the related downstream signal pathways, promotes differentiation, and induces Apoptosis. ALKBH5-IN-5 exerts excellent in vivo antitumor activity with TGITV values of 66.3%[1].

[1] Wu H, et al. Discovery of Covalent and Cell-Active ALKBH5 Inhibitors with Potent Antileukemia Effects In Vivo. Angew Chem Int Ed Engl. 2025 Feb 20:e202424928. DOI:10.1002/anie.202424928